For research use only. Not for therapeutic Use.
Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL)[1][2].
Assessment of Pharmacokinetics (PK) profile of Bcl-xL antagonist 2 (compound 14) in rat[1].
iv (1 mg/kg)
po (5 mg/kg)
CLp (mL/min/kg)
Vss (L/kg)
t 1/2 (h)
F %
0.47
0.16
6.0
16
| Catalog Number | I045493 |
| CAS Number | 1235032-75-3 |
| Synonyms | 2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-1,3-thiazole-4-carboxylic acid |
| Molecular Formula | C21H16N4O3S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H16N4O3S2/c26-18(24-20-22-15-6-1-2-7-17(15)30-20)13-5-3-4-12-8-9-25(10-14(12)13)21-23-16(11-29-21)19(27)28/h1-7,11H,8-10H2,(H,27,28)(H,22,24,26) |
| InChIKey | PHCCZZHEZZPUGG-UHFFFAOYSA-N |
| SMILES | C1CN(CC2=C1C=CC=C2C(=O)NC3=NC4=CC=CC=C4S3)C5=NC(=CS5)C(=O)O |
| Reference | [1]. Koehler MF, et al. Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL. ACS Med Chem Lett. 2014;5(6):662-667. [2]. Wang L, et al. Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor. ACS Med Chem Lett. 2020;11(10):1829-1836. |
